JPH0899858A - Skin external agent - Google Patents

Abstract

PURPOSE: To obtain skin external agent containing a water-soluble rutin and an anti-inflammatory agent as active components, having high stability and excellent anti-inflammatory and beautifying effect, and accordingly capable of exhibiting strong suppressing effect against the inflammation of skin by sunburn and the pigmentation after sunburn. CONSTITUTION: This external agent contains a water-soluble rutin [preferably, α-glycosylrutin of the formula (R is glucose, mannose, etc.); the content of rutin is 10-85wt.%] and an anti-inflammatory agent (preferably, glycyrrhizinic acid, glycyrrhetinic acid, an extract of chamomile, etc.) as active components. The content of the water-soluble rutin is preferably 0.00001-5wt.% in terms of rutin. That of the anti-inflammatory agent is preferably 0.01-3wt.%. Further, α- glycosylrutin of the formula is obtained e.g. by mixing rutin with starchiness such as dextrin followed by an enzymatic reaction.

Description

Detailed Description of the Invention

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a skin external preparation, and more particularly to a skin external preparation such as cosmetics and pharmaceuticals having excellent skin inflammation-preventing and whitening effects.

[0002]

2. Description of the Related Art Conventionally, agents having an anti-inflammatory effect such as calamine have been used to suppress skin inflammation due to sunburn, and whitening effects such as ascorbic acid and glutathione have been used to suppress pigmentation after sunburn. Each of the drugs has been used as a component of the external preparation for skin, but the external preparation for skin containing these medicinal components has a weak anti-inflammatory effect and a whitening effect, and it is hard to say that it has a sufficient sunburn preventing effect.

On the other hand, rutin is not only whole buckwheat but also potatoes, asparagus, apricots, cherries, tomatoes,
It is a compound widely contained in vegetables and fruits such as figs, citrus fruits and adzuki beans, as well as honey and green tea, and is known to have various actions such as antioxidant, UV absorption, and blood vessel reinforcement, but it is almost soluble in water. Since it was not there, it was not used very often.

Therefore, it has been attempted to enhance the water solubility of rutin and use it in a cosmetic composition (Japanese Patent Laid-Open No. 3-30083).
No. 27293, No. 3-58790, No. 3-11529.
No. 2, No. 3-275607, No. 3-275608, etc.).

[0005]

However, it is difficult to sufficiently exert the effect of water-soluble rutin alone, and it is necessary to add a large amount of water-soluble rutin in order to achieve the object.
Coloring with water-soluble rutin sometimes caused a problem in appearance.

[0006]

Therefore, the present inventors have
As a result of intensive research to obtain a skin external preparation that fully utilizes the effects of water-soluble rutin, by combining water-soluble rutin and an anti-inflammatory agent applied to the skin external preparation, the above problems are solved. However, they have found that an external preparation for skin having a synergistic effect of suppressing skin inflammation due to sunburn and pigmentation after sunburn can be obtained, and completed the present invention.

[0007] That is, the present invention provides a skin external preparation characterized by containing water-soluble rutin and an anti-inflammatory agent as active ingredients.

The water-soluble rutin which is an essential component of the present invention is
As long as the water solubility of rutin is increased as described above,
Although not particularly limited, for example, by mixing a starch substance such as dextrin with rutin and transferring glucose, maltose, maltotriose, maltotetraose or the like to rutin by an enzymatic reaction, α-represented by the general formula 1 Glycosyl rutin is preferably used. These may be used alone or in combination of two or more, and have a rutin content of 10 to 8
It is preferably 5% by weight.

[0009]

[Chemical 1]

The content of water-soluble rutin in the external preparation for skin of the present invention is preferably 0.00001 in terms of rutin.
˜5% by weight (hereinafter referred to simply as “%”) (preferably 0.0001 to 10 as powder containing unreacted dextrin)
%, More preferably 0.01 to 5%).

If the content of the water-soluble rutin as an active ingredient is less than 0.00001%, a sufficient effect may not be obtained, and if the content exceeds 5%, the effect is further increased. can not see.

On the other hand, the anti-inflammatory agent which is another essential component of the present invention includes glycyrrhizic acid, glycyrrhetinic acid, mefenamic acid, phenylbutazone, indomethacin, ibuprofen, ketoprofen, allantoin, guaiazulene and their derivatives and salts thereof. , Ε-aminocaproic acid, zinc oxide, diclofenac sodium,
Examples include licorice extract, aloe extract, shikon extract, salvia extract, arnica extract, chamomile extract, birch extract, hypericum extract, eucalyptus extract, mukurodi extract and the like.

Of these anti-inflammatory agents, glycyrrhizic acid, glycyrrhetinic acid, guaiazulene and their derivatives and salts thereof, and ε are particularly preferable.
-Aminocaproic acid, licorice extract, aloe extract,
Examples include shikon extract and chamomile extract.

The content of these anti-inflammatory agents in the external preparation for skin of the present invention is generally 0.0001 to 5%, preferably 0.01 to 3%. One or two of these anti-inflammatory agents
A combination of two or more species can be used.

The skin external preparation of the present invention can be prepared by blending the essential components, water-soluble rutin and an anti-inflammatory agent, in various forms of bases known as ordinary skin external preparations, according to a conventional method. it can.

The form of the external preparation for skin is not particularly limited, and examples thereof include cosmetics such as milky lotion, cream, lotion, pack, foundation, hair cosmetic, and cleaning agent.
It may be a dispersion, an ointment, a cream, a drug such as a liquid for external use, a quasi drug, or the like.

The base for external preparations is a base suitable for the form of these external preparations, for example, aqueous components, powders, surfactants, oils, humectants, lower alcohols and the like used in ordinary skin external preparations. If necessary, alcohols such as polyhydric alcohols, pH adjusters, preservatives, pigments, antioxidants, thickeners, fragrances, beauty ingredients and the like can be added.

[0017]

EXAMPLES Next, the present invention will be described in more detail with reference to test examples and examples, but the present invention is not limited thereto.

Test Example 1 Anti-inflammatory effect and whitening effect: A lotion containing the agents shown in Table 1 and ethanol 15% (v / v) and the remainder being purified water was prepared and applied to the back of a colored guinea pig. The effects on sunburn-induced inflammation and pigmentation were investigated. The results are shown in Table 2.

(Test method) Colored guinea pigs (10 for each group)
The back of each animal was shaved and irradiated with ultraviolet rays under anesthesia. UV irradiation is performed with Toshiba Corporation FL20S / BLB lamp and F
Three L20S / E30 lamps were simultaneously irradiated, and the amount of ultraviolet rays was 4.8 × 10 6 erg / cm 2. 0.2 ml of the sample was rubbed well into each of four places on the back of the guinea pig 24 hours before, immediately after the irradiation, and 12 hours after the irradiation, and 24 hours after the irradiation. The application site was thoroughly washed with warm water before irradiation with ultraviolet rays. The degree of inflammation was observed 24 hours after irradiation and the degree of pigmentation after 7 days.

[0021]

[Table 1]

(Evaluation criteria) Evaluation criteria for inflammation (anti-inflammatory effect) 0: No inflammation is observed 1: Very slight inflammation is observed 2: Inflammation is observed, but the boundary with the non-irradiated site is unclear 3: Inflammation was observed, and the boundary with the non-irradiated area was clear

Evaluation criteria for pigmentation (whitening effect) 0: No pigmentation is observed at all 1: Very slight pigmentation is observed 2: Pigmentation is observed, but the boundary with the non-irradiated site is unclear 3 : Pigmentation is observed, and the boundary with the non-irradiated area is clear

According to the above evaluation criteria, each score is 1
Count how many out of 10 guinea pigs are below the score,
It judged according to the following judgment criteria.

(Judgment Criteria) Among 10 animals, the number of guinea pigs with a rating of 1 point or less is 8 or more: Remarkable effect 6 or more: Effective 4 or more: Slightly effective 3 or less: Ineffective

[0026]

[Table 2]

From the results shown in Table 2, the lotion of the present invention containing water-soluble rutin and dipotassium glycyrrhizinate, guaiazulene or shikon extract is superior in anti-inflammatory effect and whitening effect to the lotion containing them alone. It is clear that

Example 1 Cream: A cream was prepared by the following formulation and the following production method. The cream of the present invention had an excellent skin inflammation preventing effect and whitening effect. <Prescription> (Amount of compounding)% (1) Polyoxyethylene monostearate (40E.O.) 2.0 (2) Glyceryl monostearate (self-emulsifying type) 5.0 (3) Stearic acid 5.0 ( 4) Behenyl alcohol 0.5 (5) Squalane 15.0 (6) Cetyl isooctanoate 5.0 (7) Butylparaben 0.1 (8) Methylparaben 0.1 (9) 1,3-Butylene glycol 5.0 ( 10) Dipotassium glycyrrhizinate (Note 1) 0.2 (11) Water-soluble rutin (Note 2) 0.5 (12) Purified water balance (13) Perfume 0.1 (Note 1) Maruzen Pharmaceutical Co., Ltd. (Note 2) ) A rutin content of 80% obtained by transferring one glucose residue to rutin

<Production Method> A. Components (1) to (7) are heated and dissolved at 70 ° C. B. Components (8) to (12) are heated and dissolved at 70 ° C. C. Add A to B and emulsify. D. Ingredient (13) is added to C and cooled to obtain a cream.

Example 2 Emulsion: An emulsion was prepared by the following formulation and the following production method. The emulsion of the present invention has an excellent effect of preventing skin inflammation and a whitening effect. <Prescription> (Blended amount)% (1) Polyoxyethylene sorbitan 1.0 monostearate (10 EO) (2) Polyoxyethylene sorbit 0.5 tetraoleate (60 EO) (3) Glyceryl Monostearate 1.0 (4) Stearic acid 0.5 (5) Behenyl alcohol 0.5 (6) Refined avocado oil 4.0 (7) Glyceryl tri-2-ethylhexanoate 4.0 (8) Butylparaben 0. 1 (9) Water-soluble rutin (Note) 0.5 (10) Guiaazulene 0.2 (11) Methylparaben 0.1 (12) Carboxyvinyl polymer 0.07 (13) 1,3-Butylene glycol 5.0 (14) ) Purified water Remainder (15) Sodium hydroxide 0.025 (16) Purified water 7.5 (17) Perfume 0.1 (Note) Rutin has one glucose residue Obtained in metastasis, of 60% by rutin content

<Manufacturing Method> A. Components (1) to (10) are heated and dissolved at 70 ° C. B. Components (11) to (14) are heated and dissolved at 70 ° C. C. Add A to B and emulsify. D. (15) to (17) are added to C and cooled to obtain a cream.

Example 3 Lotion: An emulsion was prepared by the following formulation and the following production method.
The emulsion of the present invention has an excellent effect of preventing skin inflammation and a whitening effect. <Prescription> (Blended amount)% (1) Polyoxyethylene hydrogenated castor oil (60 EO) 1.0 (2) Perfume proper amount (3) Ethanol 10.0 (4) Methylparaben 0.1 (5) ε- Aminocaproic acid 0.3 (6) Citric acid 0.1 (7) Sodium citrate 0.3 (8) 1,3-Butylene glycol 5.0 (9) Water-soluble rutin (Note) 0.01 (10) Purification Remaining water content (Note) 80% rutin content obtained by transferring one glucose residue to rutin

<Production Method> A. Components (1) to (5) are heated and dissolved at 70 ° C. B. Components (6) to (10) are heated and dissolved at 70 ° C. C. Add B to A and stir to obtain lotion.

Example 4 Cream: A cream was prepared according to the following formulation and the following production method. The cream of the present invention has an excellent effect of preventing skin inflammation,
It had a whitening effect. <Prescription> (Blended amount)% (1) Beeswax 6.0 (2) Cetanol 5.0 (3) Reduced lanolin 5.0 (4) Squalane 30.0 (5) Glycerin monostearate 4.0 (6) Lipophilic glyceryl monostearate 2.0 (7) Polyoxyethylene sorbitan mono 2.0 lauric acid ester (20 EO) (8) Water-soluble rutin (Note 1) 0.1 (9) Anti-inflammatory agent ( Note 2) (10) Preservative 0.2 (11) Perfume 0.1 (12) Purified water Remaining amount (Note 1) Obtained by transferring one glucose residue to rutin, which has a rutin content of 80%. (Note 2) Table 3 shows the compounded anti-inflammatory agents and their compounding amounts.

[0035]

[Table 3]

<Production Method> A. Ingredients (1)-(7), (10) and (11) are mixed, heated and kept at 70 ° C. B. Ingredients (8)-(9) and (12) are mixed and heated to maintain 70 ° C. C. B was added to A and mixed, and cooled to 30 ° C. to obtain a cream.

[0037]

EFFECTS OF THE INVENTION Since the external preparation for skin of the present invention has stable and excellent anti-inflammatory action and whitening action, it exerts a high inhibitory effect on skin inflammation due to sunburn and pigmentation after sunburn, and is effective for beauty and medical treatment. It is extremely useful in. that's all

Continuation of the front page (51) Int.Cl. ⁶ Identification code Internal reference number FI Technical display location A61K 7/00 K W X 7/42 31/70 ADA 35/78 C 8217-4C V 8217-4C J 8217- 4C Q 8217-4C T 8217-4C E 8217-4C

Claims (3)

[Claims] 1. A skin external preparation containing water-soluble rutin and an anti-inflammatory agent as active ingredients. 2. The external preparation for skin according to claim 1, wherein the water-soluble rutin is α-glycosyl rutin. 3. The anti-inflammatory agent is glycyrrhizic acid, glycyrrhetinic acid, mefenamic acid, phenylbutazone, indomethacin, ibuprofen, ketoprofen, allantoin, guaiazulene and their derivatives, and salts thereof, ε-aminocaproic acid, zinc oxide, diclofenac. Claims which are selected from sodium, licorice extract, aloe extract, shikon extract, salvia extract, arnica extract, chamomile extract, birch extract, hypericum extract, eucalyptus extract, mukuroji extract The external preparation for skin according to 1.